硫酸长春碱是一种细胞毒性生物碱，用于对抗各种癌症类型。硫酸长春碱抑制微管的形成并抑制 nAChR，IC50 为 8.9 μM。
| Cas No. | 143-67-9 |
| 别名 | 硫酸长春碱; Vincaleukoblastine sulfate salt |
| Canonical SMILES | CCC1(CC2CC(C3=C(CCN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)C78CCN9C7C(C=CC9)(C(C(C8N6C)(C(=O)OC)O)OC(=O)C)CC)OC)C(=O)OC)O.OS(=O)(=O)O |
| 分子式 | C46H60N4O13S |
| 分子量 | 909.05 |
| 溶解度 | ≥ 28.85 mg/mL in DMSO, ≥ 48.2 mg/mL in Water with ultrasonic |
| 储存条件 | 4°C, protect from light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Description:
IC50 Value: VIN showed EC50 values of 15 ug/ml, against P815 mastocytoma cells in-vitro[1]. Also supresses nAChR activity with IC50 of 8.9 μM.
Vinblastine can inhibit the formation of microtubule, it also inhibit nAChR. It is a anticancer drug. More and more drug combination was investigated in clinical status.
in vitro: At vinblastine concentrations of 0.5 uM and 2 uM, considerable inhibition of metabolic degradation of vinblastine was observed by competitive inhibitors of CYP3A4 (up to 60% inhibition), 2D6 (30%) and 2E1 (24%), while only a minor effect was observed for 2C9 (14%) and inhibitors of 1A2, 2C8 had no inhibitory effect on vinblastine metabolism. Vinblastine (0.5 and 2 uM) inhibited the metabolic capacity of CYP2C9 (up to 56%), 2C8 (36%), 2D6 (22%) and 3A4-mediated nifedipine oxidation (99%), while 3A4-mediated testosterone 6-beta-hydroxylation (max. 16%) as well as 1A2 and 2E1 remained unaffected[3].
in vivo: In combined intraperitoneal injection with vinblastine (200 micrograms kg-1) into P388/ADR-bearing mice, NA-382 in a suspension form (10 mg kg-1) prolonged the life-span of the mice near to that of P388/S-bearing mice treated with vinblastine alone, but verapamil even at the maximum tolerated dosage (30 mg kg-1) barely affected the in-vivo antitumour effect of vinblastine[2].
Clinical trial: Combination Chemotherapy With or Without Interleukin-2 and Interferon Alfa in Treating Patients With Metastatic Melanoma . Phase 3 Clinical |
